Acotiamide hydrate crystal form and its preparation method and use

A technology of acotiamide hydrochloride and water compound, which is applied in the application field of acotiamide hydrate and its preparation, and medicine, and can solve the problems of uncharacterized crystal structure and the like

Inactive Publication Date: 2015-03-25
TIANJIN HANKANG PHARMA BIOTECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

[0010] Patent WO1996036619 discloses a method for synthesizing acotiamide hydrochloride, but this patent only discloses its synthesis method, a

Method used

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  • Acotiamide hydrate crystal form and its preparation method and use
  • Acotiamide hydrate crystal form and its preparation method and use
  • Acotiamide hydrate crystal form and its preparation method and use

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0052] Add 60 grams of acotiamide hydrochloride and 300 milliliters of water into a 500 ml reaction flask equipped with stirring, a thermometer and a condenser, add 0.5 grams of dimethylformamide (DMF) to the above aqueous solution, and stir for 30 minutes. Filter and cool the filtrate to 13°C for later use.

[0053] Cool 1000ml of acetone-ethanol=6:4 mixed solution to 13°C, add the above standby solution while stirring, keep it warm for 18 hours, crystals precipitate, filter, and dry to obtain 55.8 grams of white crystals. Measured 3 times by Karl Fischer method, get the average value, contain 8.94% (percentage by weight) of moisture. Purity 99.9% (HPLC normalization method), optical purity 99.96% ee (chiral HPLC).

[0054] Elemental Analysis Results:

[0055] Measured value (calculated value), C: 47.15(47.10), H: 6.94(6.92), N: 10.45(10.47),

[0056] S: 5.95 (5.98), Cl: 6.60 (6.64)

[0057] X-ray powder diffraction characteristic absorption peaks (2θ) and D values ​​are ...

Embodiment 2

[0062] Tablets containing acotiamide hydrochloride trihydrate

[0063] Prescription: 20 grams of acotiamide hydrochloride trihydrate, 100 grams of lactose, 36 grams of corn starch, 30 grams of crystalline cellulose, 10 grams of carboxypropyl cellulose, and 4 grams of magnesium stearate.

[0064] The ingredients described above were uniformly mixed, and the mixture was formed into 100 mg / tablet tablets with a single punch tablet machine through a hole of 9.1 mm.

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Abstract

The invention belongs to the technical field of medicine and relates to an Acotiamide hydrochloride hydrate crystal form and a preparation method thereof. The Acotiamide hydrochloride contains trihydrate and has the advantages of chemical purity of 99.9%, the largest impurity content less than 0.1%, optical purity of 99.95%ee and good stability. The invention also relates to a use of the Acotiamide hydrochloride hydrate composition in preparation of drugs for treating stomach reception disorder.

Description

technical field [0001] The invention belongs to the technical field of medicine, and in particular relates to acotiamide hydrate and a preparation method thereof, and also relates to the application of the composition of the compound in the manufacture of medicines for treating gastric accommodation disorders. Background technique [0002] Gastrointestinal motility is an extremely complex and highly coordinated nerve-muscle activity, mainly controlled by the efferent and afferent nerves of the enteric nervous system, and its propulsive movement is regulated by many factors such as nerves and body fluids, including acetylcholine, dopamine, 5- Neurotransmitters such as serotonin and motilin can increase gastrointestinal motility by acting on one of them. Gastrointestinal motility disorders can lead to a variety of gastrointestinal symptoms, typical manifestations are gastric, esophageal or duodenal reflux, heartburn, gastritis, esophagitis, functional dyspepsia, constipation, ...

Claims

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Application Information

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IPC IPC(8): C07D277/56A61K31/426A61P1/14
CPCC07D277/56
Inventor 严洁李轩
Owner TIANJIN HANKANG PHARMA BIOTECH
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